928006-47-7

Upstream product

• 612-41-9 2-nitrocinnamic acid 
• 88939-75-7 methyl β-(o-aminophenyl)acrylate 
• 39228-29-0 methyl 2-nitrocinnamate 
• 839672-50-3 methyl 3-[2-((4-biphenyl)iminomethyleneamino)phenyl]acrylate 
• 954-81-4 N-(5-bromopentyl)phthalimide 
• 111-24-0 1,5-dibromo-pentane 
• 928006-41-1 2-(5-(pyrrolidin-1-yl)pentyl)isoindoline-1,3-dione 
• 928006-42-2 t-butyl (5-pyrrolidin-1-ylpentyl)carbamate 
• 928006-43-3 N-methyl-5-(pyrrolidin-1-yl)pentan-1-amine 
• 71302-71-1 5-(pyrrolidin-1-yl)pentan-1-amine 
• 928006-45-5 KYS₀₅₀₇₉ 

Relevant academic research and scientific papers

3,4-DIHYDROQUINAZOLINE DERIVATIVES

The present invention relates to 3,4-dihydroquinazoline derivatives, a process of preparing them and a pharmaceutical composition including them. The 3,4-dihydroquinazoline derivatives of the present invention have excellent T-type calcium channel blocking effect and anti-cancer activity.

Synthesis and SAR study of T-type calcium channel blockers. Part II

3,4-Dihydroquinazoline derivatives have been known to be the novel and potent T-type calcium channel blockers. From a systematic variation of 3,4-dihydroquinazoline derivative 5c (KYS05043), plausible SAR results were established. It was revealed that a 5-(dimethylamino)pentylamino group at R 1, a biphenyl group at R2, and a benzyl amido group at R3 in the 3,4-dihydroquinazoline backbone are closely related with the channel selectivity (T/N-type) as well as the potency based on the discovery of 6k (KYS05090).

T-type Ca2+ channel blockers suppress the growth of human cancer cells

In order to further clarify the role of T-type Ca2+ channels in cell proliferation, we have measured the growth inhibition of human cancer cells by using our potent T-type Ca2+ channel blockers. As a result, KYS05090, a most potent T-type Ca2+ channel blocker, was found to be as potent as doxorubicin against some human cancer cells without acute toxicity. Therefore, this letter provides the biological results that T-type calcium channel is important in regulating the important cellular phenotype transition leading to cell proliferation, and thus novel T-type Ca2+ channel blocker presents new prospects for cancer treatment.

Synthesis and biological evaluation of novel T-type calcium channel blockers

3,4-Dihydroquinazoline analogues substituted by N-methyl-N-(5-pyrrolidinopentyl)amine at the 2-position were synthesized and their blocking effects were evaluated for T- and N-type calcium channels. Compound 11b (KYS05080), compared to mibefradil (IC50 = 1.34 ± 0.49 μM), was about 5-fold potent (IC50 = 0.26 ± 0.01 μM) for T-type calcium channel (α1G) blocking and its selectivity of T/N-type was also improved (7.5 versus 1.4 of mibefradil).